Acetylcholinesterase Inhibitive Activity-Guided Isolation of Two New Alkaloids from Seeds of Peganum Nigellastrum Bunge by an In Vitro TLC- Bioautographic Assay

作者：Zheng Xi yuan; Zhang Zi jia; Chou Gui xin; Wu Tao; Cheng Xue mei; Wang Chang hong^*; Wang Zheng tao

来源：Archives of Pharmacal Research, 2009, 32(9): 1245-1251.

DOI：10.1007/s12272-009-1910-x

• Peganum nigellastrum Bunge
• Acetylcholinesterase
• TLC-bioautographic assay
• Alzheimer's disease
• Alkaloid
• Nigellastrine I
• Nigellastrine II

Acetylcholinesterase inhibitors (AChEIs) currently form the basis of the newest drugs available for the treatment of Alzheimer's disease. For the aim of screening effective AChEIs, the methanol extracts of the seeds of genus Peganum were found to show significant inhibitory activity of acetylcholinesterase enzyme (AChE) using an in vitro TLC-bioautographic assay. In further studies to seed of P. nigellastrum Bunge, activity-guided fractionation led to the isolation of two new alkaloids nigellastrine I (9) and nigellastrine II (10), and along with eight known alkaloids, vasicinone (1), vasicine (2), harmine (3), deoxyvasicinone (4), deoxyvasicine (5), harmaline (6), harmol (7), harman (8), in which harmol and harman were first isolated from species P. nigellastrum Bunge. As active constituents, all compounds showed good inhibitory activities against AM. The results of in vitro semi-quality TLC-bioautographic assay showed that harmine, harmaline and harmol displayed a similar AChE inhibitive activities comparing to galanthamine. These results indicated that these alkaloids in P. nigellastrum Bunge could be a potent class of AChEIs.

• 出版日期2009-9
• 单位上海中医药大学; 上海中药标准化研究中心